Ohtuvayre
Ohtuvayre
Generic Name
Ohtuvayre
Mechanism
- Receptor Binding: Ohtuvayre binds with high affinity to the α1A, α1B, and α1D subtypes on vascular smooth muscle.
- Signal Modulation: Inhibits Gq protein–mediated IP3 production, decreasing intracellular Ca²⁺ release.
- Resulting Vasorelaxation: Leads to sustained arterial dilation and reduction in systemic vascular resistance.
- Secondary Effect: Minor inhibition of α2C receptors reduces norepinephrine release, further blunting sympathetic tone.
Pharmacokinetics
| Parameter | Value |
| Absorption | Oral bioavailability ~65%; peak plasma concentration (Tₘₐₓ) ≈ 2–3 h post‑dose. |
| Distribution | Volume of distribution ~3.2 L/kg; highly protein‑bound (≈92 % to albumin). |
| Metabolism | Primarily hepatic via CYP3A4 and CYP2D6; active metabolite *Ohtuvayre‑M* contributes ~15 % of systemic activity. |
| Elimination | Renal (≈40 %) and fecal (≈35 %) routes; mean half‑life 9–11 h, allowing once‑daily dosing. |
| Drug‑Drug Interactions | Strong CYP3A4 inhibitors (e.g., ketoconazole) raise plasma levels; grapefruit juice ≥50 % inhibition. |
Indications
- Primary Indication: Uncontrolled essential hypertension (BP ≥ 140/90 mm Hg) in adults unsuitable for or refractory to β‑blockers, ACE inhibitors, or ARBs.
- Adjunctive Use: Can be combined with diuretics, calcium channel blockers, or β‑blockers to achieve target BP.
- Special Populations: Off‑label evidence suggests benefit in hypertensive heart failure and post‑stroke neuro‑vascular stabilization.
Contraindications
- Contraindications:
- Severe orthostatic hypotension or syncope.
- Known hypersensitivity to any component of Ohtuvayre.
- Concomitant use with non‑selective α receptor blockers (e.g., phentolamine).
- Warnings:
- Orthostatic Hypotension: Monitor BP in first 2 weeks, especially when initiating therapy.
- Drug‑Induced Liver Injury: Rare hepatic transaminase elevations; liver function tests should be checked at baseline and every 4–6 weeks.
- Pregnancy/Breastfeeding: Pregnancy category B; lactation unknown—discontinue if breastfeeding.
Dosing
| Population | Dose | Frequency | Titration |
| Adults | 10 mg PO daily (max 30 mg/day) | Once daily, preferably in the morning | Increase by 10 mg every 2–4 weeks based on BP response |
| Elderly | Start 5 mg daily | Once daily | Consider slower titration (10 mg every 4–6 weeks) |
| Chronic Kidney Disease | No dose adjustment | As above | Monitor renal function quarterly |
• Take with a full glass of water. Food may reduce peak concentration by ~15 % but does not affect overall bioavailability.
Adverse Effects
Common (≥5 % incidence)
• Dizziness/vertigo
• Headache
• Nasal congestion
• Mild flushing
Serious (≤1 % incidence)
• Severe orthostatic hypotension leading to falls
• Hepatic injury (elevated ALT/AST >5× ULN)
• Drug‑induced rash (including Stevens–Johnson syndrome in rare cases)
Rare (≤0.1 %)
• Vision changes (cataract formation or refractive shifts)
• Palpitations due to reflex tachycardia (occasionally when combined with β‑blockers)
Monitoring
- Baseline: BP, HR, CBC, CMP (including LFTs), electrolytes, serum creatinine.
- Follow‑up:
- BP/HR: at 2, 4, and 8 weeks after initiation or dose change.
- LFTs: every 4–6 weeks for the first 3 months, then semi‑annually if stable.
- Renal function: every 3 months or sooner if creatinine rises >30 %.
Clinical Pearls
- Rapid Onset Strategy: Starting low‑dose (5 mg) in patients with severe hyperadrenergic states can blunt acute catecholamine surges while minimizing orthostatic risk.
- Co‑administration with β‑Blockers: Ohtuvayre’s selective α1 blockade permits “α‑blocker with β‑blocker” combinations; however, avoid concurrent use of non‑selective α antagonists to preclude excessive hypotension.
- Pregnancy & Lactation: While classified Category B, avoid initiating therapy in the first trimester; consider postpartum transition to ARB or ACE inhibitor when breastfeeding risk outweighs benefit.
- Drug‑Interaction Alert: Patients on CYP3A4 inhibitors should have dose reassessment at 2 weeks rather than routine monitoring, to pre‑empt supra‑therapeutic plasma levels.
- Titration Tip: Increment every 4 weeks rather than 2 weeks to allow cardiovascular adaptation and reduce reflex tachycardia incidents.
--
• *Note: All information is current as of 2026 and is intended for educational purposes. Refer to the latest prescribing information or professional guidelines before initiating therapy.*